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Assay Detail

CHEMBL4821060

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Binding
Binding affinity to histamine H3 receptor (unknown origin)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect.
Gao L, Hao C, Chen J, Ma R, Zheng L, Wu Q, Liu X, Liu BF, Zhang G, Chen Y, Jin J.
Bioorg Med Chem Lett (2021) 40 : 127909 -127909
PubMed 33705900 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 6.96 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4865907 1 8.09
CHEMBL4846866 1 8.04
CHEMBL4861193 1 7.92
CHEMBL4861311 1 7.87
CHEMBL4867978 1 7.85
CHEMBL4861643 1 7.80
CHEMBL4852663 1 7.03
CHEMBL4857350 1 6.95
CHEMBL4879054 1 6.90
CHEMBL4853342 1 6.83
CHEMBL4873319 1 6.83
CHEMBL4877940 1 6.82
CHEMBL4856753 1 6.82
CHEMBL4863980 1 6.79
CHEMBL4877973 1 6.79
CHEMBL4870716 1 6.78
CHEMBL4878271 1 6.73
CHEMBL4860828 1 6.71
CHEMBL4870307 1 6.59
CHEMBL4859348 1 6.57
CHEMBL4857918 1 6.57
CHEMBL4865735 1 6.57
CHEMBL4876719 1 6.50
CHEMBL85 RISPERIDONE 4.0 1 5.96
CHEMBL1112 ARIPIPRAZOLE 4.0 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4865907 Ki = 8.2 nM 8.09
CHEMBL4846866 Ki = 9.2 nM 8.04
CHEMBL4861193 Ki = 11.9 nM 7.92
CHEMBL4861311 Ki = 13.4 nM 7.87
CHEMBL4867978 Ki = 14.0 nM 7.85
CHEMBL4861643 Ki = 15.8 nM 7.80
CHEMBL4852663 Ki = 93.7 nM 7.03
CHEMBL4857350 Ki = 112.6 nM 6.95
CHEMBL4879054 Ki = 125.3 nM 6.90
CHEMBL4853342 Ki = 148.7 nM 6.83
CHEMBL4873319 Ki = 147.2 nM 6.83
CHEMBL4877940 Ki = 151.2 nM 6.82
CHEMBL4856753 Ki = 153.2 nM 6.82
CHEMBL4863980 Ki = 163.4 nM 6.79
CHEMBL4877973 Ki = 163.7 nM 6.79
CHEMBL4870716 Ki = 166.3 nM 6.78
CHEMBL4878271 Ki = 187.0 nM 6.73
CHEMBL4860828 Ki = 195.5 nM 6.71
CHEMBL4870307 Ki = 256.0 nM 6.59
CHEMBL4859348 Ki = 270.1 nM 6.57
CHEMBL4857918 Ki = 270.7 nM 6.57
CHEMBL4865735 Ki = 269.5 nM 6.57
CHEMBL4876719 Ki = 312.3 nM 6.50
CHEMBL85 RISPERIDONE Ki = 1105.5 nM 5.96
CHEMBL1112 ARIPIPRAZOLE Ki = 2361.0 nM 5.63